- Valemetostat
-
- $96.00 / 1mg
-
2025-05-27
- CAS:1809336-39-7
- Min. Order:
- Purity: 98.77%
- Supply Ability: 10g
- Valemetostat
-
- $96.00 / 1mg
-
2025-05-27
- CAS:1809336-39-7
- Min. Order:
- Purity: 98.77%
- Supply Ability: 10g
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| | DS-3201 Basic information |
| Product Name: | DS-3201 | | Synonyms: | DS-3201;(R)-7-chloro-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-((1r,4R)-4-(dimethylamino)cyclohexyl)-2,4-dimethylbenzo[d][1,3]dioxole-5-carboxamide;Valemetostat;1,3-Benzodioxole-5-carboxamide, 7-chloro-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethyl-, (2R)-;inhibit,DS 3201,DS3201,Histone Methyltransferase,Inhibitor,T-cell,Valemetostat,lymphoma;Valemetostat (DS-3201);VALEMETOSTAT (DS-3201) (DS-3201B);(R)-7-Chloro-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-(trans-4-(dimethylamino)cyclohexyl)-2,4-dimethylbenzo[d][1,3]dioxole-5-carboxamide | | CAS: | 1809336-39-7 | | MF: | C26H34ClN3O4 | | MW: | 488.02 | | EINECS: | | | Product Categories: | | | Mol File: | 1809336-39-7.mol |  |
| | DS-3201 Chemical Properties |
| Boiling point | 610.0±55.0 °C(Predicted) | | density | 1.26±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: soluble | | form | A crystalline solid | | pka | 11.87±0.10(Predicted) | | color | White to off-white |
| | DS-3201 Usage And Synthesis |
| Uses | Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma[1][2][3]. | | in vivo | Valemetostat (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training[2]. | Animal Model: | Male C57BL/6J mice with chronic and acute running exercise or without exercise[1] | | Dosage: | 0.01 mg/g | | Administration: | Intraperitoneal injection; 0.01 mg/g; 30 min before the start of running exercise | | Result: | Significantly increased the level of H3K27me3 , slightly decresed EZH1 level , upregulated the EZH2 level and increased the level of phosphorylated AMPK after exercise. Repressed myonuclear H3K27me3 accumulation during training and caused a failure of adaptive changes.
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| | IC 50 | EZH1 | | References | [1] Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.
[2] Shimizu J, Kawano F. Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice. J Physiol. 2022 Jul;600(14):3331-3353. DOI:10.1113/JP282917
[3] Yamagishi M, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019 Nov 19;29(8):2321-2337.e7. DOI:10.1016/j.celrep.2019.10.083 |
| | DS-3201 Preparation Products And Raw materials |
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